Safinamide mesylate

Cas No.:	202825-46-5
Chemical Name:	Deudextromethorphan; CTP-786; D6-Dextromethorphan; d6-DM; AVP-786，AVP 786，AVP786
Synonyms:	Deudextromethorphan; CTP-786; D6-Dextromethorphan; d6-DM; AVP-786，AVP 786，AVP786
SMILES:	C[C@H](NCC1=CC=C(OCC2=CC=CC(F)=C2)C=C1)C(N)=O.CS(=O)(O)=O
Formula:	C18H23FN2O5S
M.Wt:	398.45

Description:	Safinamide mesylate mesylate (FCE 26743 mesylate; EMD 1195686 mesylate) is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
In Vivo:	Safinamide mesylate (intraperitoneal injection; 90 mg/kg; once daily; 14 days) treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice[3]. Safinamide mesylate (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release in vivo. At the dose 30 mg/kg, Safinamide mesylate prevents the effect of veratridine both on Glu (treatment F1,8=1.31; time×treatment interaction F8,64=2.4) and GABA (treatment F1,8=4.04; time F8,64=3.76, time×treatment interaction F8,64=2.83) release. Safinamide mesylate causes a slight, albeit not significant, reduction of veratridine-stimulated Glu release at 0.5 mg/kg and full inhibition at 5 and 15 mg/kg in rat[3].
In Vitro:	Safinamide mesylate (1-300 µM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When currents are stimulated to a Vtest of +10 mV from a Vh of -110 mV, the IC50 value was 262 µM. When the holding potential is depolarized to -53 mV, the inhibitory effect of Safinamide mesylate with a lower IC50 value (8 µM) in rat cortical neurons[1].